MER-128|CAS |DC Chemicals

Cas No.:
Chemical Name:	MER-128

Cat. No.	Product name	Field of application
DC55130	CDK4 inhibitor compound 12	CDK4 inhibitor compound 12 is a novel inhibitor of CDK4 with the activity 97 μM.
DC73181	XPW1	XPW1 is a potent and selective CDK9 inhibitor with excellent anti-ccRCC activity and low toxicity.
DC73179	SW394703	SW394703 is a novel DDB1-dependent molecular glue degrader for cyclin K, SW394703 is toxic to HCT116 cells (IC50=1.2 uM).
DC73175	NCGC00131308	NCGC00131308 is a small molecule inhibitor that effectively disrupts IQGAP1-Cdc42 interaction in breast cancer cells, shows EC50 of 4.47 uM in biochemical HTRF assays.
DC73171	ISM042-2-048	ISM042-2-048 is a potent, selective inhibitor of cyclin-dependent kinase 20 (CDK20, cell cycle-related kinase/CCRK) with IC50 of 33.4 nM (CDK20/CycT1), Kd value of 566 nM.
DC73170	GFH009	GFH009 is a potent, selective CDK9 inhibitor, inhibits the activity of the CDK9/cyclin T1 regulatory complex of P-TEFb.
DC73166	Cyclin K degrader DS17	Cyclin K degrader DS17 is a selective cyclin K molecular glue degrader with TR-FRET EC50 of 19 nM.
DC70984	(S)-CR8	(S)-CR8 is the S-isomer of CR8. (S)-CR8 is a potent and selective CDK inhibitor with IC50s of 0.060, 0.080, 0.11, 0.12, and 0.15 μM for CDK2/cyclin E, CDK2/cyclin A, CDK9/cyclin T, CDK5/p25, and CDK1/cyclin B, respectively. (S)-CR8 reduces SH-SY5Y cells survival (IC50 0.40 μM).
DC70766	Senexin C	Senexin C is a novel potent, selective and orally bioavailable CDK8/19 inhibitor with Kd of 1.4 and 2.9 nM for CDK8/CycC and CDK19/CycC, respectively.Senexin C inhibits CDK8/CycC with IC50 of 3.6 nM, shows high selectivity against other HDAC isoforms.Senexin C is more metabolically stable and provides a more sustained inhibition of CDK8/19-dependent cellular gene expression when compared with the prototype inhibitor Senexin B.Senexin C inhibits MV4-11 leukemia growth in a systemic in vivo model with good tolerability.
DC70298	CDDD11-8	CDDD11-8 is a potent CDK9 inhibitor co-targeting FLT3-ITD with Ki values of 8 and 13 nM, respectively.CDDD11-8 displays excellent kinome selectivity in a panel of 369 human kinases.CDDD11-8 displays antiproliferative activity against leukemia cell lines, and particularly potent effects against MV4-11 and MOLM-13 cells, which are known to harbor the FLT3-ITD mutation and mixed lineage leukemia (MLL) fusion proteins.CDDD11-8 causes a robust tumor growth inhibition by oral administration in animal xenografts, induces tumor regression at dose of 125 mg/kg.